ST1936 oxalate
Based on 1 publication(s) in Google Scholar
ST1936 oxalate is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 oxalate also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor.
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- CAS. Nr.: 1782228-83-4
- Formel: C15H19ClN2O4
- Molecular Weight:326.78
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Speicherung:
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) ST1936 oxalate
MoreAlle 5-HT Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
5-HT6 Receptor 13 nM (Ki) |
5-HT2B Receptor |
5-HT6 Receptor |
5-HT7 Receptor |
Human 5-HT7 Receptor 168 nM (Ki) |
5-HT2B Receptor 245 nM (Ki) |
α1-adrenergic receptor 390 nM (Ki, rat) |
α2-adrenergic receptor 300 nM (Ki, rat) |
α2-adrenergic receptor 300 nM (Ki, human) |
In Vitro
ST1936 oxalate appears to be relatively selective for 5-HT6 receptors, although it has shown affinity also for 5-HT2B, 5-HT1A, 5-HT7 receptor and α-adrenergic receptors when tested in a broad crossreactivity panel that comprised G-protein-coupled receptors, ion channel binding sites, enzymes, and transporters[1].
ST1936 oxalate behaves as a full 5-HT6 agonist on cloned cells and is able to increase Ca2+ concentration, phosphorylation of Fyn kinase, and regulate the activation of ERK1/2 that is a downstream target of Fyn kinase[2].
ST1936 oxalate reduces the frequency of spontaneous excitatory postsynaptic currents, with an IC50 of 1.3 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
ST1936 (5, 10, 20 mg/kg; i.p.) oxalate increases extracellular DA and NA levels in the nucleus accumbens (NAc) core. Doses of 10 mg/kg increases dialysate DA (peak: 179%) while higher dose increases both DA and NA dialysates (201% and 231%, respectively). Doses of 5 mg/kg does not produce any effect[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1782228-83-4
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Molecular Weight 326.78
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Formel C15H19ClN2O4
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SMILES
CC(N1)=C(CCN(C)C)C2=C1C=CC(Cl)=C2.O=C(O)C(O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Biochem Biophys Res Commun
Structural insight into the selective agonist ST1936 binding of serotonin receptor 5-HT6. [Abstract]2023 Sep 3:671:327-334. PMID: 37327704
Reinheit & Dokumentation
Verweise
[1]. Borsini F, et al. Effects of ST1936, a selective serotonin-6 agonist, on electrical activity of putative mesencephalic dopaminergic neurons in the rat brain. J Psychopharmacol. 2015 Jul;29(7):802-11. [Content Brief]
[2]. Riccioni T, et al. ST1936 stimulates cAMP, Ca2+, ERK1/2 and Fyn kinase through a full activation of cloned human 5-HT6 receptors. Eur J Pharmacol. 2011;661(1-3):8-14. [Content Brief]
[3]. Tassone A, et al. Activation of 5-HT6 receptors inhibits corticostriatal glutamatergic transmission. Neuropharmacology. 2011;61(4):632-637. [Content Brief]
[4]. Valentini V, et al. A microdialysis study of ST1936, a novel 5-HT6 receptor agonist. Neuropharmacology. 2011;60(4):602-608. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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